ICGM, Montpellier University, CNRS, ENSCM, Montpellier, France.
Int J Pharm. 2019 Oct 30;570:118516. doi: 10.1016/j.ijpharm.2019.118516. Epub 2019 Jul 15.
This study aims to prove the value of the polyoxazolines polymer family as surfactant in formulations for topical application and as an alternative to PEG overuse. The amphiphilic polyoxazolines (POx) were demonstrated to have less impact on cell viability of mice fibroblasts (NIH3T3) than their PEG counterparts. Mixed micelles, made of POx and phosphatidylcholine, were manufactured using thin film and high pressure homogenizer process. The mixed micelles were optimized to produce nanosized vesicles of about 20 nm with a spherical shape and stable over 28 days. The natural lipophilic antioxidant, quercetin, was successfully encapsulated (encapsulation efficiency 94 ± 4% and drug loading 3.6 ± 0.2%) in the mixed micelles with no morphological variation. Once loaded in the formulation, the quercetin impact on cell viability of NIH3T3 was decreased while its antioxidant activity remained unchanged. This work highlights the capacity of amphiphilic POx to create, in association with phospholipids, stable nanoformulations which show promise for topical delivery of antioxidant and ensure skin protection against oxidative stress.
本研究旨在证明聚恶唑啉聚合物家族作为表面活性剂在局部应用配方中的价值，并作为 PEG 过度使用的替代品。与聚乙二醇 (PEG) 相比，两亲性聚恶唑啉 (POx) 对小鼠成纤维细胞 (NIH3T3) 的细胞活力影响更小。采用薄膜法和高压匀质法制备了由 POx 和磷脂组成的混合胶束。对混合胶束进行了优化，使其在 28 天内稳定地产生约 20nm 的纳米级球形囊泡。天然亲脂性抗氧化剂槲皮素成功地包封在混合胶束中（包封效率为 94±4%，载药量为 3.6±0.2%），且形态无变化。一旦加载到制剂中，槲皮素对 NIH3T3 细胞活力的影响降低，而其抗氧化活性保持不变。这项工作强调了两亲性 POx 与磷脂结合形成稳定的纳米制剂的能力，这为抗氧化剂的局部递送提供了前景，并确保皮肤免受氧化应激的保护。
